Department of Chemistry, University of Connecticut , Storrs, Connecticut 06269, United States.
J Am Chem Soc. 2017 May 10;139(18):6278-6281. doi: 10.1021/jacs.6b13087. Epub 2017 Apr 25.
Herein we describe a nucleic acid functionalized nanocapsule in which nucleic acid ligands are assembled and disassembled in the presence of enzymes. The particles are fully degradable in response to esterases due to an embedded ester cross-linker in the particle's core. During synthesis the nanocapsules can be loaded with hydrophobic small molecules and post self-assembly undergo covalent cross-linking using copper catalyzed click chemistry. They can then be functionalized with thiolated DNA through stepwise thiolyne chemistry using UV light irradiation. Additionally, the capsule is compatible with enzyme mediated functionalization of a therapeutic mRNA-cleaving DNAzyme at the particle's surface. The resulting particle is highly stable, monodisperse in size, and maximizes the therapeutic potential of both the particles interior and exterior.
在此，我们描述了一种核酸功能化的纳米胶囊，其中核酸配体在酶的存在下进行组装和拆卸。由于颗粒核心中的嵌入酯交联剂，颗粒可完全响应酯酶进行降解。在合成过程中，纳米胶囊可以负载疏水分子，并且在自组装后可以使用铜催化点击化学进行共价交联。然后可以通过使用紫外光照射逐步硫醇点击化学将巯基化 DNA 官能化到胶囊上。此外，该胶囊与酶介导的治疗性 mRNA 切割 DNA 酶在颗粒表面的功能化兼容。得到的颗粒非常稳定，尺寸单分散，并最大限度地提高了颗粒内部和外部的治疗潜力。
